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  • Title: Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.
    Author: Hidaka K, Kimura T, Tsuchiya Y, Kamiya M, Ruben AJ, Freire E, Hayashi Y, Kiso Y.
    Journal: Bioorg Med Chem Lett; 2007 Jun 01; 17(11):3048-52. PubMed ID: 17400453.
    Abstract:
    Based on a highly potent allophenylnorstatine-containing inhibitor, KNI-10006, against the plasmepsins of Plasmodium falciparum, we synthesized a series of tripeptide-type compounds with various N-terminal moieties and evaluated their inhibitory activities against plasmepsin II. Certain phenylacetyl derivatives exhibited extremely high affinity with K(i) values of less than 0.1n M suggesting successful hydrophobic interactions.
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